BMS quinoline PAR4 antagonists show strong oral exposure in rats
- A Bristol-Myers Squibb team reports a quinoline-based series of PAR4 antagonists, found through iterative structure-activity optimization, that reaches very high potency against the target.
- The compounds also show favorable oral exposure and peak plasma levels in rats, which supports further development as antithrombotic agents.
💡 Points Based on the abstract
Potency plus rat oral exposure is a decent start, but that's all this tells me. For an antithrombotic target the whole game is the window between antiplatelet effect and bleeding, and nothing here speaks to it. I'd want PAR1 selectivity, human versus rodent activity, and any efficacy data before getting excited about the quinoline.